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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-M1069
M1069

Chemical Structure : M1069

CAS No.: 2459881-03-7

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M1069 (M-1069)

货号: PC-49354Not For Human Use, Lab Use Only.

M1069 (M-1069) is a potent, dual antagonist of the A2A and A2B adenosine receptors, with selectivity of >100 fold against the A1 and A3 receptors.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    M1069 (M-1069) is a potent, dual antagonist of the A2A and A2B adenosine receptors, with selectivity of >100 fold against the A1 and A3 receptors.
    M1069 caused a dose-dependent suppression of 5′-N-ethylcarboxamide adenosine (stable analog of adenosine)-stimulated cAMP and pCREB induction and rescue of IL-2 production (A2A readout) in assays with primary human T cells.
    M1069 also suppressed VEGF production from human macrophages (A2B readout) in adenosine-rich settings.
    M1069 exhibited superior suppression of protumorigenic cytokine secretion, including CXCL1, CXCL5 and granulocyte-colony stimulating factor, and the rescue of IL12 secretion from adenosine-differentiated dendritic cells, as compared to an A2Aselective antagonist.
    M1069 demonstrated superior T cell activation in adenosine-differentiated dendritic cells.
    M1069 reduced tumor growth as a monotherapy and enhanced anti-tumor activity with chemotherapeutic agents in a murine CD73hi/adenosine-rich 4T1 syngeneic breast tumor model.

    物理化学性质&存储条件

    分子量 430.523
    分子式 C21H26N4O4S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (S)-N-(7-(3,6-dihydro-2H-pyran-4-yl)-4-methoxythiazolo[4,5-c]pyridin-2-yl)-7-oxa-2-azaspiro[4.5]decane-2-carboxamide

    参考文献

    1. Rinat Zaynagetdinov, et al. Cancer Res (2022) 82 (12_Supplement):3499.

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